The sixteen anticonvulsant drugs marketed in the United States provide significant seizure relief for only 50-75% of epileptic patients. The therapeutic effects are sometimes accompanied by serious side effects such as sedation, ataxia, psychoses, suicidal depression, gastrointestinal disturbances, gingival hyperplasia, lymphadenopathies, megaloblastic anemias, hepatotoxicity, nephropathies, hirsutism, and fetal malformations. These side effects, which range in severity from mild sedation to death from aplastic anemia, are particularly troublesome since most of the marketed anticonvulsants have very low therapeutic ratios. For example, phenytoin, one of the most widely used anticonvulsants, controls seizures in man only when plasma levels reach 10 mcg./ml. Toxic effects such as nystagmus are seen at around 20 mcg./ml., ataxia is obvious at 30 mcg./ml., and lethargy is apparent at about 40 mcg./ml. See "The Pharmacological Basis of Therapeutics" (Gilman, Goodman, and Gilman, ed., 6th Ed., MacMillan Publishing Co., Inc., New York, New York (1980)), p. 455. In view of these facts, most epileptologists indicate there is a definite need for more selective and less toxic anticonvulsant drugs.
U.S. Pat. No. 4,150,153 teaches certain 1-(naphthylethyl)-imidazole derivatives which are taught to be useful as anticonvulsant and antisecretory agents. See also J. Med. Chem., 24, 67 (1981). A variety of naphthyl- and phenylalkyl imidazoles are taught to be anticonvulsants in U.S. Pat. No. 4,275,071. See also J. Med. Chem., 24, 727 (1981).
Certain fluorenylazolylmethylcarbinols are taught to be useful as antimycotic agents in U.S. Pat. No. 4,239,765. This publication teaches certain of the ketone compounds used in the present invention as intermediates to the claimed tertiary carbinol antimycotic agents.